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Bioorg Med Chem Lett. 2004 Sep 6;14(17):4445-8.

Discovery of inhibitors of human adipocyte fatty acid-binding protein, a potential type 2 diabetes target.

Author information

1
Department of Medicinal Chemistry, Biovitrum AB, SE-751 37 Uppsala, Sweden.

Abstract

Low micromolar human A-FABP inhibitors were found by utilizing a fluorescence polarization assay, X-ray crystallography and modeling. The carbazole- and indole-based inhibitors displayed approximately 10-fold preferences over human H-FABP and E-FABP, and are highly selective against I-FABP. This communication describes the SAR for drug-like synthetic inhibitors of human A-FABP.

PMID:
15357969
DOI:
10.1016/j.bmcl.2004.06.057
[Indexed for MEDLINE]

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